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  4. Tanespimycin

Tanespimycin  (Synonyms: 17-AAG; NSC 330507; CP 127374)

製品番号: HY-10211 純度: 99.07%
COA 取扱説明書

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Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.

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Tanespimycin 構造式

Tanespimycin 構造式

CAS 番号 : 75747-14-7

容量 価格（税別） 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 79 在庫あり
Solution
10 mM * 1 mL in DMSO USD 79 在庫あり
Solid
5 mg USD 46 在庫あり
10 mg USD 72 在庫あり
25 mg USD 120 在庫あり
100 mg USD 300 在庫あり
200 mg USD 420 在庫あり
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 40 publication(s) in Google Scholar

Tanespimycin 関連抗体

Top Publications Citing Use of Products

顧客検証

WB
IHC

    Tanespimycin purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2023 Apr;51(4):32.  [Abstract]

    Tanespimycin (17‑AAG) inhibits the levels of HSP90 and NLRP3, and decreases GSDMD expression, in MH‑S cells.

    Tanespimycin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Mar 27;37(1):70.  [Abstract]

    Cells are first treated with commercially available HIF-1α inhibitors, including compounds targeting Top1 (Camptothecin, CPT), Top2 (VP; MX) and HSP90 (17-AAG) as well as 2-ME, and then subjected to Western blotting analysis.

    Tanespimycin purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Feb 7;9(2):165.  [Abstract]

    Western blot analysis of Hsp70 protein and Hsp90 client proteins IKK and EGFR after 24 h Tan IIA treatment. The Hsp90 inhibitor 17-AAG (10 μM) is included as a positive control

    Tanespimycin purchased from MedChemExpress. Usage Cited in: Front Mol Neurosci. 2018 Nov 6;11:401.  [Abstract]

    Effects of 17-AAG on neurogenesis 4 weeks after SAH.

    Tanespimycin purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2016 Sep;15(9):2107-18.  [Abstract]

    Combination of MDV3100 and 17-AAG leads to decreased AR protein level and transcriptional activity. (A&B) LNCaP (A) and C4-2 (B) cells are treated as indicated for 24 hr, followed by IB against AR, PSA and CHIP. (C&D) 22RV1 (C) and MR49F (D) cells are treated as indicated for 24 hr, followed by IB against AR and HSP90. (E) C4-2 cells are treated as indicated for 24 hr, fractionated into cytoplasm and nuclear, followed by IB against AR and Plk1.

    HSP アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

    Antibiotic アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

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    製品説明

    Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90[1][5]. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression[3].

    IC50 & Target[5]

    HSP90

    5 nM (IC50)

    Autophagy

     

    Mitophagy

     

    体外実験

    Tanespimycin causes the degradation of HER2, Akt, and both mutant and wild-type AR and the retinoblastoma-dependent G1 growth arrest of prostate cancer cells. Tanespimycin inhibits prostate cancer cell lines with IC50s ranged from 25-45 nM (LNCaP, 25 nM; LAPC-4, 40 nM; DU-145, 45 nM; and PC-3, 25 nM)[1].
    Tanespimycin (0.1-1 μM) induces a nearly complete loss of ErbB2 on ErbB2-overexpressing breast cancer cells[2]. Tanespimycin inhibits cell growth and induces G2/M cell cycle arrest and apoptosis in CCA cells together with the down-regulation of Bcl-2, Survivin and Cyclin B1, and the up-regulation of cleaved PARP[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Tanespimycin 関連抗体
    体内実験

    Tanespimycin (25-200 mg/kg, i.p.) causes a dose-dependent decline in AR, HER2, and Akt expression in prostate cancer xenografts. Tanespimycin treatment at doses sufficient to induce AR, HER2, and Akt degradation results in the dose-dependent inhibition of androgen-dependent and -independent prostate cancer xenograft growth without toxicity[1].
    Tanespimycin (60 mg/kg) with Rapamycin (30 mg/kg) inhibits A549 and MDA-MB-231 tumor growth and effects tumor cures in MDA-MB-231 tumor-bearing animals by tail vein injection[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    585.69

    分子式

    C31H43N3O8
    CAS 番号
    Appearance

    Solid

    SMILES

    O=C(C(NC(/C(C)=C/C=C\[C@H](OC)[C@H](/C(C)=C/[C@@H]([C@H]([C@H](C[C@@H](C1)C)OC)O)C)OC(N)=O)=O)=CC2=O)C1=C2NCC=C
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (85.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7074 mL 8.5369 mL 17.0739 mL
    5 mM 0.3415 mL 1.7074 mL 3.4148 mL
    10 mM 0.1707 mL 0.8537 mL 1.7074 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (8.54 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 5 mg/mL (8.54 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.07%

    COA (251 KB) HNMR (273 KB) LCMS (263 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [1]

    For the Alamar Blue proliferation assay, 2-4×103 cells are plated in 96-well plates. Later (48 h), cells are treated with Tanespimycin for 96 h or 0.01% DMSO as control. On day 4, Alamar Blue viability assay is performed as described elsewhere. IC50 and IC90s are calculated as the doses of Tanespimycin required to inhibit cell growth by 50 and 90%, respectively. Cell cycle distribution is assayed as described previously with a Becton Dickinson fluorescence-activated cell sorter and analyzed by the Cell Cycle Multicycle system.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [1]

    Tanespimycin is dissolved in an EPL vehicle. To aid in the identification of an optimal dose and schedule, nontumor bearing mice are treated by i.p. injection with 25-200 mg/kg of Tanespimycin 5 days/week for 3 weeks or by the EPL vehicle alone. Serum samples are taken from each group, and equal volumes are pooled on days 5, 10, and 15 of treatment for serum chemistry and liver function analysis. At sacrifice, plasma samples are collected for complete blood count. A gross necropsy is performed on all of the mice, and a complete necropsy, including histopathology, is performed on 1 animal/group.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7074 mL 8.5369 mL 17.0739 mL 42.6847 mL
    5 mM 0.3415 mL 1.7074 mL 3.4148 mL 8.5369 mL
    10 mM 0.1707 mL 0.8537 mL 1.7074 mL 4.2685 mL
    15 mM 0.1138 mL 0.5691 mL 1.1383 mL 2.8456 mL
    20 mM 0.0854 mL 0.4268 mL 0.8537 mL 2.1342 mL
    25 mM 0.0683 mL 0.3415 mL 0.6830 mL 1.7074 mL
    30 mM 0.0569 mL 0.2846 mL 0.5691 mL 1.4228 mL
    40 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0671 mL
    50 mM 0.0341 mL 0.1707 mL 0.3415 mL 0.8537 mL
    60 mM 0.0285 mL 0.1423 mL 0.2846 mL 0.7114 mL
    80 mM 0.0213 mL 0.1067 mL 0.2134 mL 0.5336 mL
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    Tanespimycin Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Tanespimycin75747-14-717-AAG NSC 330507 CP 127374NSC330507NSC 330507NSC-330507CP127374CP 127374CP-127374HSPAutophagyMitophagyBacterialApoptosisAntibioticHeat shock proteinsMitochondrial AutophagyARHER2A549MDA-MB-231tumorprostatecancerstk38Inhibitorinhibitorinhibit

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    製品名:
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